Available on line at : www.eijppr.com International Journal of Pharmaceutical and Phytopharmacological Research

ISSN (Online) 2249 – 6084 ISSN (Print) 2250 – 1029 Int.J.Pharm.Phytopharmacol.Res. 2012, 1(6): 391-395 (Review Article)

A Comprehensive Review on conyzoides Linn.(Goat weed)

Tailor Chandra Shekhar*1, Goyal Anju 2

*1Division of Pharmaceutical Sciences, Shri Guru Ram Rai Institute of Technology and Science, Patel Nagar, Dehradun-248001, Uttarakhand, India. 2 Bhupal Nobel’s Girls College of Pharmacy, Udaipur-313001, Rajasthan, India.

Received on: 10/05/2012 Accepted on: 25/05/2012

ABSTRACT Linn.(Family: ) a medicinal as a whole was commonly known as Goat weed or Appa grass is widely distributed over the tropical and subtropical regions of the world. It is an annual branching herb which grows up to 1 m in height. The stems and leaves are covered with fine white hairs. A wide range of chemical compounds including alkaloids, flavonoids, chromenes, benzofurans and terpenoids have been isolated from this species. Extracts and metabolites from this plant have been found to possess pharmacological and insecticidal activities. Ageratum conyzoides is used in various parts of Africa, Asia and South America for curing various diseases in the folk medicine. It is used as a purgative, febrifuge, against colic, skin ulcers, as an antienteralgic and antipyretic, for cuts as a wound dressing.

Keywords: Ageratum conyzoides; Flavonoids; Chromenes; Benzofurans; Alkaloids; Terpenoids, Bioactivity.

INTRODUCTION Ageratum conyzoides has bioactive activity that may have Since ancient times are used as rich source of agricultural use, as shown by several research investigations medicine. Scientific exploration of traditional knowledge of in different countries. Pereira in 1929, cited by Jaccoud use of herbs in treatment of various ailments is one of the (1961), reported use of the leaves as an insect (moth) thrust areas of research. Herbal medicines are in great repellent. The insecticide activity may be the most important demand in the developed as well as developing countries for biological activity of this species 4. Ageratum is derived primary healthcare because of their wide biological and from the Greek "a geras," meaning non-aging, referring to medicinal activities, higher safety margins and lesser costs. the longevity of the or the whole plant. The specific Ageratum conyzoides is widely utilized in traditional epithet "conyzoides" is derived from "kónyz," the Greek medicine systems wherever it grows, although applications name of Inula helenium,which it resembles. The presence vary by region. Traditional communities in India use this of Ageratum conyzoides can also be used as an seed plant as a bacteriocide, antidysenteric, and antilithic. and in inhibitor, decreasing development of several herbaceous Asia, South America and Africa, aqueous extract of this plants. an aqueous extract of the aerial part or roots of this plant is used as a bacteriocide 1. In Central Africa it is used species (15 g of aerial part or 3 g of roots in 100 ml of to treat pneumonia, but the most common use is to cure water, during 24 h) inhibited germination of wheat and rice wounds and burns. Ageratum conyzoides is also utilized to seeds. It grows well on wastelands and in fields after the treat fever, rheumatism, headache and colic. The medicinal rainy season 5. value of this plant in the treatment of a large number of human ailments is mentioned in Ayurveda, Charaka Samhita SYNONYMS and Sushruta Samhita 2. Hindi : Jangli pudina, uchunti; English: Goat weed, It is an annual branching herb which grows to approximately Billygoat weed,Chicken weed ; Spanish (El Salvador): 1 m in height. The stems and leaves are covered with fine Mejorana, sunsumpate (Columbia): Yerba hemostatica white hairs, the leaves are ovate and up to 7.5 cm long. The Portuguese: Mentrasto, Tropic ageratum flowers are purple to white, less than 6 mm across and African Vernacular Names arranged in close terminal inflorescences. The fruits are West Africa (Igbo): Nri-ewu (Yoruba): Imieshu , yarnigbei. achene and are easily dispersed. The plant grows commonly in the proximity of habitation, thrives in any garden soil and TAXONOMICAL CLASSIFICATION is very common in waste places and on ruined sites 3. It has Kingdom : Plantae a peculiar odor likened in Australia to that of a male goat Subkingdom : Angiosperm and hence its name ‘goat weed’ or ‘ billy goat weed’. Class: 391 Chandra Shekhar Tailor et al...... Int.J.Pharm.Phytopharmacol.Res. 2012, 1(6): 391-395 Order: dimethylchromene-7-O-glucopyranoside(13), 6-(1- Family:Asteraceae methoxyethyl).-7-methoxy-2,2-dimethylchromene(3),6-(1- Genus:Ageratum hydroxyethyl)-7-methoxy-2,2 dimethylchromene(4), 6-(1- Species:conyzoides ethoxyethyl).-7-methoxy-2,2-dimethylchromene(5) , 6- Binomial name: Ageratum conyzoides Linn. angeloyloxy-7-methoxy-2,2-dimethylchromene(8) and an inseparable mixture of encecanescins(20-22). Benzofuran BOTANICAL DESCRIPTION derivatives, 2(2’-methylethyl)-5,6dimethoxybenzofuran(17), Ageratum conyzoides (Fig.1) is a small herbaceous plant 14-hydroxy-2H, β-3-dihydroeuparine(18) as well as belongs to the family Asteraceae. It is softly hairy, erect, chromone derivatives, 3-(2-methylpropyl)-2-methyl-6,8- branched, annual weed up to 80‐90 cm in height. It is a dimethoxychrom-4-one(15) and 2-(2 methylprop-2-enyl.-2- tropical plant used in various parts of Africa, Asia and South methyl-6,7-dimethoxychroman-4-one(16) have also been America for curing various diseases. The stems and leaves reported from the plant 8. are covered with fine white hairs; the leaves are ovate and up to 7.5 cm long. The flowers are purple to white, less than Ageratum conyzoides is rich in polyoxygenated flavonoids, 6 mm across and arranged in a terminal inflorescence. The 21 of them have been reported in the whole plant. Among fruits are achaenes and easily dispersed.Because of its them there are 14 polymethoxylated flavones(23-36). These propagation it become a weed and causes problems for polyhydroxyflavones include quercetin, kaempferol and farmers and ecologists. Seeds are positively photoblastic, their glycosides, too. The two major common sterols and viability is often lost within 12 months. It is not eaten by sitosterol and stigmasterol together with minor sterol were men because of its bad odour, like a male goat and is named isolated together with the triterpene friedelin(41). Other goat weed or billy goat weed.The whole plant is only used common substances are sesamine, fumaric acid, caffeic acid, for medicinal purposes and has a long history in the folk phytol, and long chain hydrocarbons. The medicine of different countries 6. polyhydroxyflavones include scutellarein-5,6,7,4_- tetrahydroxyflavone, quercetin, quercetin-3- PHYTOCHEMICAL CHARACTERISTICS rhamnopiranoside(37), kaempferol, kaempferol -3- There is high variability in the secondary metabolities of A. rhamnopiranoside(38-39) and kaempferol 3,7- conzyoide which include flavonoids, alkaloids, cumarins, diglucopiranoside . The isoflavone obtained from the plant essential oils, and tannins. Many of these are biologically was reported by a group of Indian researchers 8-9.The active. The oil content varies randomly from 0.11 to 0.58% chemical structures of all above phytoconstituents are for leaves and from 0.03 to 0.18% for the roots depending represented in Fig.2-5. on times of the year .From water distillation of the fresh flowers, the oil content was found to be 0.2% . The yield of PHARMACOLOGICAL ACTIVITIES oil from the petroleum ether extract of the seed was 26%.A Crude extract large number of constituents have been identified from the It has been found to have neuromuscular blocking activity. GC-MS analysis of the essential oil of Ageratum conyzoides The leaf extract has been used in the treatment of chronic 7-8. The largest so far, a total of 51 constituents have been pain in osteoarthrotic patients . Its antimicrobial and reported from the analysis of an oil sample of the plant. The anticonvulsant activities have also been demonstrated . The constituents identified include 20 monoterpenes 6.4% and methanolic extract of the whole plant also has antimicrobial 20 sequiterpenes 5.1%. The mono- and the sesquiterpenes activity. The analgesic activity of the leaf extract was are obtained in minute quantities trace-0.1%. The detected by hot plate method10. monoterpenes obtained in approximately 1% of the oil include sabinene and β-pinene, 1.6%, β-phellandrene, 1,8- Essential oil cineole and limonene, 2.9%, terpinen-4-ol, 0.6%, and α- Essential oil of A. conyzoides has been tested for anti- terpineol, 0.5%. Ocimene which is found in trace amount in inflammatory, analgesic and antipyretic activities in mice the oil from the Nigerian plant, is found to be 5.3% of the oil and rats. At doses of 3 and 4 ml kg per os, the oil was found from the plant collected in India. α -Pinene 6.6%, eugenol to have a significant anti-inflammatory (cotton pellet 4.4% and methyleugenol 1.8% are also obtained from the granuloma) activity11. Indian plant oil 8. Metabolites The most common component of the essential oil of Pharmacological activities of the most significant Ageratum conyzoides is 7-methoxy2,2- dimethylchromene metabolites, besides the essential oil from this plant, (precocene-I)(1). Other related compounds obtained from responsible for the medicinal properties have not been the oil include encecalin(6), 6-vinyl-7-methoxy-2,2- identified. There are, however, a wide spectrum of dimethylchromene(7), dihydroencecalin(9), pharmacological activities of the classes of compounds dihydrodemethoxyencecalin(10), demethoxyencecalin(11), obtained from this plant. For example, simple chromenes demethylencecalin(12) and 2(1-oxo-2-methylpropyl.-2- and chromans especially the 6-amino and 6-acetamido methyl-6,7-dimethoxychromene(14). The presence ofthese derivatives have been reported to have anti-depressant, acetyl chromenes in Ageratum conyzoides is believed to be analgesic and antipyretic properties 12-13. Other simple 2,2- of chemotaxonomic significance 8. dimethyl chromene derivatives like 6(1-hydroxyethyl.)-7,8- dimethoxy-2,2-dimethylchromene and 6-hydroxy-7,8- In addition to the chromenes obtained from the oil, seven dimethoxy-2,2 dimthyl chromene have been shown to have other chromene derivatives are isolated from hexane extract antimicrobial activities. The sterols, especially stigmasterol, of the aerial part of the plant. These are 2,2- have been shown to exert significant anti- inflammatory activity. The flavonoids possess a wide range of biological 392 Chandra Shekhar Tailor et al...... Int.J.Pharm.Phytopharmacol.Res. 2012, 1(6): 391-395 activities. The free radical scavenging and anticancer CONCLUSION activities of the flavonoids are of public knowledge13. Even Ageratum conyzoides has been widely studied. It is believed though the biological activities of the flavonoids isolated that a detailed information as presented in this review on its from Ageratum conyzoides have not been investigated. phytochemistry and various biological properties of the extracts and the constituents might provide incentive for Some of the important pharmacological properties exhibited proper evaluation of the use of the plant in medicine and in by Ageratum conyzoides Linn includes: agriculture. Further work, however, still needs to be carried out on the toxicity of the plant and especially on some A)Antibacterial effects flavonoids as Quericitin, which have been shown in few Water and ethanol extracts of the shredded fresh collected cases to cause antilithiatic effect in rats. plant were investigated for antibacterial activity. In an in vitro anti-methicillin resistant Staphylococcus aureus test (MRSA) the minimum inhibition concentration (MIC) 30.6 to 43.0 and 45.4 to 71.0 µg/kg were recorded for ethanol and water extracts. The minimum bactericidal concentration (MBC) was higher for both extracts.

B)Anti inflammatory effects A hydroalcoholic extract was studied for anti inflammatory effects in rats. A group of rats, orally treated with 250 mg/kg extract had a 38.7 % reduction in the cotton pellet-induced granuloma. The development of chronically induced paw edema was also reduced significantly by the plant extract.

C)Wound healing effects The wound healing effect of the Ageratum conyzoides methanolic extract was studied in Wistar rats (n=10). Fig.1: Ageratum conyzoides Linn., Asteraceae Wounds prepared in excised areas of the skin were packed with gauze soaked by the extracts and were determined histologically after 10 days. The Ageratum sections showed fewer inflammatory cells and more fibrosis than controls 14.

D)Spasmolytic effects and gastro protection The ethanol extract of Ageratum conyzoides was evaluated for gastroprotection in rats using the ibuprofen, ethanol and cold restraint ulcer stress model. Efficacy was assessed by determination of mean ulcer size, ulcer numbers and an ulcer index 15.

E)Antitumour activity In a murine ascites Dalton´s lymphoma in vivo the aqueous extract of Ageratum conyzoides roots decreased glutathion in the liver and in the lymphoma cells of the tumour-bearing mice 16.

INSECTICIDAL ACTIVITIES Ageratum conyzoides has bioactivity that may have agricultural use. The insecticidal activity may in fact be the most important biological activity of this species. Both the essential oil as well as the major components of the oil, namely the precocenes, have been reported to have antijuvenile hormonal activity 17.

ALLELOPATHY Both the volatile oil and the aqueous extract of the Ageratum conyzoides have been shown to have allelopathic effects on a number of cultivated crops. The saturated aqueous solution of the isolated and purified precocene I and II have been reported to have significant inhibitory effect on the seedling growth of radish, tomato and ryegrass. The allelopathic potential of the aqueous extract from different Fig.2: Phytochemical structures (1-18) organs of Ageratum conyzoides and from its different development stages especially from different habitats, was different 18-20. 393 Chandra Shekhar Tailor et al...... Int.J.Pharm.Phytopharmacol.Res. 2012, 1(6): 391-395

Fig.5: Phytochemical Structures (41-47)

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394 Chandra Shekhar Tailor et al...... Int.J.Pharm.Phytopharmacol.Res. 2012, 1(6): 391-395 15) Silva MJ, Capaz FR, Vale MR, Effects of the water soluble 19) Kong,C,Hu,F,Xu,X, Allelopathic poential and Chemical fraction from leaves of Ageratum conyzoides on smooth constituents of volatiles from Ageratum conyzoides under muscle, Phytother Research, 2000, 14(2), 130-2. stress, J Chem Ecol, 2002, 28(6), 1773-82. 16) Shirwaikar A, Bhilegoankar PM, Malini S, Kumar JS, The 20) http://www.mmh- gastroprotective activity of the ethanol extract of Ageratum mms.com/downloads/mp03ageratumconyzoides.pdf conyzoides,J Ethnopharmacol, 2003, 86(1),117-121. accessed on March,2012. 17) Achola,KJ,et.al, Bronchodilating and uterine activities of Ageratum conyzoides extract, Pharmaceutical Biology, *Corresponding Author: 1998, 36(2), 93-96. Mr. Chandra Shekhar Tailor 18) Nyunai, N, et.al, Antihyperglycaemic effect of Ageratum conyzoides L. fractions in Norglycemic and diabetic male Lecturer, Division of Pharmaceutical Sciences, wistar rats, International Journal of Biomed.and SGRRITS, Dehradun,Uttarakhand, India. Pharma.sciences, 2010,4(1), 38-42. Email: [email protected]

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